16219-10-6Relevant articles and documents
Synthesis and evaluation of a full-agonist orvinol for PET-imaging of opioid receptors: [11C]PEO
Marton, János,Schoultz, Bent W.,Hjoernevik, Trine,Drzezga, Alexander,Yousefi, Behrooz H.,Wester, Hans-Jurgen,Willoch, Frode,Henriksen, Gjermund
, p. 5586 - 5589 (2009)
Antagonist radiotracers have shown only a low sensitivity for detecting competition from high-efficacy agonists at opioid receptors (ORs) in vivo. We report that [11C]PEO binds with high affinity to μ and κ-opioid receptors, is a full agonist, and concentrates in brain regions of rats with a high density of the μ-OR after intravenous injection. Blocking studies with μ and κ-OR selective compounds demonstrated that the binding of [11C]PEO is saturable and selective to the μ-OR in rat brain.